Department of Bioengineering, University of Utah, Salt Lake City, UT 84112, USA.
Macromol Biosci. 2012 Apr;12(4):502-14. doi: 10.1002/mabi.201100350. Epub 2012 Jan 25.
A monoclonal antibody (mAb) to P-glycoprotein (Pgp), UIC2, is used as a targeting moiety for N-(2-hydroxypropyl)methacrylamide (HPMA) copolymer/drug [(meso chlorin e(6) mono(N-2-aminoethylamide) (Mce(6)) or doxorubicin (DOX)] conjugates to investigate their cytotoxicity towards the Pgp-expressing human ovarian carcinoma cell line A2780/AD. The binding, internalization, and subcellular trafficking of a fluorescein labeled UIC2 targeted HPMA copolymer are studied and show localization to the plasma membrane with limited internalization. The specificity of the UIC2-targeted HPMA copolymer/drug conjugates are confirmed using the sensitive cell line A2780 that does not express Pgp.
一种针对 P 糖蛋白(Pgp)的单克隆抗体(mAb)UIC2 被用作 N-(2-羟丙基)甲基丙烯酰胺(HPMA)共聚物/药物[间-氯代(六)单(N-2-氨基乙基酰胺)(Mce(6))或阿霉素(DOX)]缀合物的靶向部分,以研究它们对表达 Pgp 的人卵巢癌细胞系 A2780/AD 的细胞毒性。研究了荧光素标记的 UIC2 靶向 HPMA 共聚物的结合、内化和细胞内转运,并显示其定位于质膜,内化有限。使用不表达 Pgp 的敏感细胞系 A2780 证实了 UIC2 靶向 HPMA 共聚物/药物缀合物的特异性。